JP2001302479A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for oral cavity by blending an active ingredient having bactericidal and anti-bacterial effects without losing its activity in a temperature sensitive sol gel transition preparation consisting mainly of a block copolymer of a polyoxyethylene and polyoxypropylene. SOLUTION: This composition for oral cavity is characterized by incorporating hinokithiol into an aqueous solution containing the block copolymer of a polyoxyethylene and polyoxypropylene and having 0-50 deg.C sol gel transition temperature.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to an oral composition containing a block copolymer of polyoxyethylene and polyoxypropylene.

[0002]

2. Description of the Related Art Heretofore, incorporation of an active ingredient into a system in which a large amount of a surfactant is present involves forming a complex with the surfactant or incorporating the active ingredient into micelles. It was inactivated and it was very difficult to mix the active ingredient while maintaining the activity. For example, when an anionic surfactant and a cationic germicide are used in combination for a mouthwash or the like, a complex is formed to cause scumming and deactivation.
Therefore, in order to avoid this complex formation, a nonionic surfactant such as a polyoxyethylene / polyoxypropylene block copolymer (hereinafter also referred to as Pluronic) is used. However, in this case,
It is known that although a complex is not formed, the formation can be suppressed, but the bactericide is incorporated into the micelles and is completely inactivated by adding a small amount thereof. On the other hand, it is well known that a high-concentration aqueous solution of pluronic enters a sol state on a low temperature side and a gel state on a high temperature side from an LCST (lower critical solution temperature). It has been proposed to apply this property to use as a drug delivery system (DDS) for gelling Pluronic at body temperature. However, since a large amount of Pluronic is actually used, even if the active ingredient incorporated in the micelle is drug-delivered, it is not possible to sufficiently exert its efficacy. As described above, it has been a major problem to mix the Pluronic sol-gel transition preparation without deactivating the active ingredient.

[0003]

DISCLOSURE OF THE INVENTION The present invention eliminates an active ingredient having a bactericidal and antibacterial effect in a temperature-sensitive sol-gel transfer preparation containing a block copolymer of polyoxyethylene and polyoxypropylene as a main component. It is an object of the present invention to mix without utilizing the active ingredient.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies in order to solve the above-mentioned problems, and as a result, it has been found that hinokitiol has a temperature which is mainly composed of a block copolymer of polyoxyethylene and polyoxypropylene. The present inventors have found that active compounding can be carried out without inactivation in a sensitive sol-gel transfer preparation, and the present invention has been accomplished. That is, according to the present invention, an oral solution characterized by containing hinokitiol in an aqueous solution containing a block copolymer of polyoxyethylene and polyoxypropylene and having a sol-gel transition temperature of 0 to 50 ° C. Compositions are provided.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION A block copolymer of polyoxyethylene and polyoxypropylene (hereinafter simply referred to as a copolymer) used in the present invention comprises a polyoxyethylene portion and a polyoxypropylene portion. The proportion of the polyoxyethylene moiety contained in the molecule is 50 to 90%, preferably 55 to 85%. The number average molecular weight of this copolymer is 5,000 to 20,000, preferably 8,000 to
15,000. The oxypropylene moiety has a number average molecular weight of 1,000 to 5,000, preferably 15 to 5,000.
00 to 4500.

The oral composition of the present invention comprises an aqueous solution of the above-mentioned copolymer. In this case, the concentration of the copolymer in the aqueous solution is 5 to 40%, preferably 10 to 30%. The sol-gel transition temperature of the aqueous copolymer solution used in the present invention is 0 to 50 ° C, preferably 5 to 45 ° C.
The transition temperature can be adjusted by appropriately setting the amount and grade of the copolymer.

The hinokitiol used in the present invention includes natural tropolone isolated from phenolic components of essential oils such as cypress plants such as Taiwan cypress, scented cypress, musk, asnaro, and cypress, and juniper. In the present invention, not only such natural products but also synthetic products may be used as hinokitiol. It is also possible to use an extract or powder containing hinokitiol. For example, hinoki oil, hinoki powder, hiba oil, hiba powder and the like can be mentioned.

[0008] The oral cosmetic of the present invention may optionally contain an abrasive, provided that it does not inhibit its sol-gel transition.
Thickeners, binders, surfactants, sweeteners, flavors, preservatives and the like can be added. As the abrasive, conventionally known ones, for example, silica-based abrasives such as precipitated silica, silica gel, aluminosilicate and zirconosilicate; dibasic calcium phosphate dihydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide , Alumina, magnesium carbonate, tertiary magnesium phosphate, titanium oxide, zeolite, aluminum silicate, zirconium silicate, and a synthetic resin-based abrasive. These abrasives can be used alone or in combination of two or more. Examples of the thickener include glycerin, sorbitol, propylene glycol, polyethylene glycol and the like.

Examples of the binder include sodium carboxymethylcellulose, carrageenan, sodium hydroxyethylcellulose, sodium alginate, propylene glycol alginate, xanthan gum, polyacrylic acid, sodium polyacrylate, tarragant gum, guar gum, locust bean gum, hydroxyethylcellulose, hydroxyethylcellulose Propyl cellulose, gellan gum, gelatin, curdlan, gum arabic, agar,
Pectin, polyvinyl alcohol, polyvinylpyrrolidone, pullulan and the like. As the surfactant, an anionic surfactant, a cationic surfactant, a nonionic surfactant, and the like can be blended. Specifically, sodium lauryl sulfate, sodium α-olefin sulfonate, N-acyl Glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyglycerin fatty acid ester, polyoxyethylene sorbitan monostearate, etc. Can be

As sweeteners, sorbitol, xylitol, erythritol, maltitol, lactitol,
Aspartame, saccharin sodium, stevioside, stevia extract, paramethoxycinamic aldehyde, neohesperidyl hydrochalcone, perillartin and the like can be mentioned. Flavors include peppermint oil, spearmint oil, amis oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil Natural flavors and menthol, such as lime oil, lavender oil, rosemary oil, laurel oil, camomill oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, etc.
Carvone, anethole, cineol, methyl salicylate,
Single fragrances such as cinnamic aldehyde, eugenol, thymol, linalool, linalool acetate, limonene, menthone, menthyl acetate, pinene, octyl aldehyde, citral, pulegone, carbyl acetate, anisaldehyde, etc., as well as ethyl acetate, ethyl butyrate, allyl cyclohexane Strawberry flavor of a mixed flavor including individual flavors and / or natural flavors such as propinate, methyl anthranilate, ethyl methyl glyceride, vanillin, undecalactone, hexanal, ethyl alcohol, propyl alcohol, butanol, isoamyl alcohol, and apple. Flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, tropical fruit flavor, butterf Ba, milk flavor, can be used a known perfume used Fruit Mix flavors like, the oral composition is not limited to perfume embodiment. Examples of the coloring agent include Blue No. 1, Yellow No. 4, and titanium dioxide.

[0011] The oral composition of the present invention is an aqueous composition, and such a composition includes a mouthwash, a liquid dentifrice, a mouthwash and the like.

[0012]

According to the present invention, hinokitiol having a bactericidal and antibacterial effect is deactivated in a temperature-sensitive sol-gel transition preparation containing a block copolymer of polyoxyethylene and polyoxypropylene as a main component. The present invention provides an oral composition formulated without any additives.

[0013]

EXAMPLES The present invention will now be described specifically with reference to examples and comparative examples, but the present invention is not limited to the following examples. The evaluation test method is as follows.

Example 1, Comparative Examples 1-3 Pluronic A 19%, fungicide 0.2%, ethanol 7
% And a water balance, the sol-gel transition temperature of this aqueous solution was examined, and its bactericidal effect was examined as follows. Table 1 shows the results. The Pluronic A (BASF, trade name "F-10")
8 ") are as follows. (1) Number average molecular weight: 16250 (2) Number average molecular weight of polyoxypropylene part: 325
0 (3) Ratio of polyoxyethylene part: 80% (sterilization test) A test sample diluted 2.5 times (3 ml) was added to P.O. gingivalis suspension 30μ
L is added, and the mixture is kept at 37 ° C. (10 minutes) immediately after stirring. After 10 minutes, the mixture was diluted to 10 ⁵ with physiological saline, each diluted solution was applied to a THB blood plate, anaerobically cultured at 37 ° C. for 5 days, and the number of colonies was counted. Table 1 shows the results. The results in the table are represented by Log values.

[0015]

[Table 1] From the results shown in Table 1, it was found that in the case of the composition of the present invention, hinokitiol was incorporated without deactivation.

Hereinafter, specific examples of the composition of the present invention will be described. Example 2 Pluronic F-98 (manufactured by BASF, number average molecular weight 13750, number average molecular weight of polyoxypropylene part 2750, ratio of polyoxyethylene part 80%) 17 (%) ethanol 7 hinoki oil 0.01 citric acid 0 0.05 sodium citrate 0.3 water balance sol-gel transition temperature 39 (° C.) This composition showed high antibacterial and bactericidal activities.

Example 3 Pluronic F-98 (manufactured by BASF, number average molecular weight 13300, number average molecular weight of polyoxypropylene part 4000, proportion of polyoxyethylene part 70%) 17 (%) ethanol 7 Hinoki powder 0.5 Sodium benzoate 0.3 Citric acid 0.05 Sodium citrate 0.3 Fragrance 0.5 Water balance Sol-gel transition temperature 28 (° C) This composition showed high antibacterial and bactericidal activities.

Example 4 Pluronic F-127 10 (%) Pluronic F-68 (manufactured by BASF, number average molecular weight 9600, number average molecular weight of polyoxypropylene part 1920, ratio of polyoxyethylene part 80%) 4 ethanol 7 Hiba oil 0.2 Tranexamic acid 0.05 Xylitol 5 Sodium benzoate 0.3 Citric acid 0.05 Sodium citrate 0.3 Fragrance 0.5 Water Balance Sol-gel transition temperature 36 (° C) This composition has high antibacterial properties. It showed bactericidal activity.

Example 5 Pluronic F-108 10 (%) Pluronic F-88 (manufactured by BASF, number average molecular weight 13750, number average molecular weight of polyoxypropylene part 2750, ratio of polyoxyethylene part 80%) 5 ethanol 7 Hiba powder 0.2 Vitamin E 0.1 Vitamin B6 0.1 Tranexamic acid 0.05 Xylitol 5 Sodium benzoate 0.3 Citric acid 0.04 Sodium citrate 0.3 Fragrance 0.5 Water Balance Sol-gel transition temperature 29 ( ° C) This composition showed high antibacterial and bactericidal activities.

 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Haruo Kadoya 1-3-7 Honjo, Sumida-ku, Tokyo F-term in Lion Corporation (reference) 4C083 AA112 AB052 AC102 AC132 AC302 AC312 AC622 AD051 AD052 AD551 AD552 AD632 AD662

Claims (1)

[Claims] 1. An oral composition comprising a block copolymer of polyoxyethylene and polyoxypropylene, wherein hinokitiol is contained in an aqueous solution having a sol-gel transition temperature of 0 to 50 ° C. .